Bamlanivimab (Anti-Human SARS-CoV-2) is the first COVID-19 monoclonal antibody (mAb) to be granted Emergency Use Authorization (EUA) in November 2020 by the U.S. Food and Drug Administration (FDA). However, Bamlanivimab is withdrawn in April 2021 following the rise of SARS-CoV-2 virus variants resistant to Bamlanivimab[1].
PLpro-IN-1 (Compound 2) is a SARS-CoV PLpro inhibitor (IC50: 8.7 μM). PLpro-IN-1 can be used for antiviral research[1].
AT-9010 tetrasodium, a triphosphate active metabolite of AT-527, is a potent inhibitor of NiRAN (a function essential for viral replication). AT-9010 tetrasodium can inhibit SARS-CoV-2 replication[1].
Alunacedase alfa (HrsACE2; GSK 2586881) is a human recombinant soluble angiotensin-converting enzyme-2 (hrsACE2). Alunacedase alfa is a genetically modified soluble form of ACE2, it decreases cell entry of SARS-CoV-2 competing for membrane-bound ACE2. Alunacedase alfa has the potential for the research of SARS-CoV-2[1][2].
4'-O-Methylbavachalcone is a chalcone isolated from Psoralea corylifolia, inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) papain-like protease (PLpro) activity, with an IC50 of 10.1 μM[1].
HCoV-OC43-IN-1 (Compound IV-16) is a coronavirus HCoV-OC43 inhibitor. HCoV-OC43-IN-1 has antiviral efficacy (EC50: 90 nM). HCoV-OC43-IN-1 inhibits the mRNA level and expression of viral nucleocapsid protein (NP)[1].
Hydroxychloroquine sulfate is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling.
SARS-CoV-2 nsp13-IN-3 (Compound C3) is a SARS-CoV-2 non-structural protein 13 (nsp13) small-molecule inhibitor with an IC50 of 32 μM against nsp13 ssDNA+ ATPase[1].
Rimteravimab (XVR011) is a bivalent VHH-Fc antibody with potent neutralizing activity with high stability, broad coverage and silenced Fc effector functions against the disease caused by SARS-CoV-2[1].
SARS-CoV-2 nsp13-IN-1 (compound C1) is a potent nsp13 (non-structural protein 13) inhibitor. SARS-CoV-2 nsp13-IN-1 only inhibits nsp13 ssDNA+ ATPase, with an IC50 of 6 μM. SARS-CoV-2 nsp13-IN-1 does not inhibit ssDNA- ATPase. SARS-CoV-2 nsp13-IN-1 can be used for COVID-19 research[1].
SSAA09E3 is a SARS-CoV entry inhibitor that inhibits SARS/HIV pseudotyped virus entry with an EC50 of 9.7 μM in 293T cells and inhibits SARS-CoV infection of Vero cells with an EC50 of 0.15 μM[1][2].
AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[1][2].
SARS-CoV-2 3CLpro-IN-2 (Compound 1) is a potent inhibitor of 3CL protease. SARS-CoV-2 3CLpro-IN-2 has the potential for the research of SARS-CoV-2 diseases[1].
Astodrimer (SPL7013 free base) is a large (3-4 nm, ~ 16.5 kDa), negatively charged, highly-branched dendrimer, is a potent virucidal agent. Astodrimer shows antiviral and virucidal activity against a broad spectrum of viruses, including SARS-CoV-2, HIV-1, HSV-1, HSV-2, HPV. Astodrimer also has antibacterial properties[1][2][3].
Novel inhibitor of SARS-CoV replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2)
Indinavir sulfate ethanolate (MK-639 ethanolate) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate ethanolate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate ethanolate is also a SARS-CoV 3CLpro inhibitor[1][2][3][4].
Methisazone (Marboran) is an antiviral agent that works by inhibiting mRNA and protein synthesis. Methisazone is also a SARS-CoV-2 (COVID-19) inhibitor. Methisazone is mainly used in pox viruses[1].
Tixagevimab (AZD8895) is a human monoclonal antibody that targets the SARS-CoV-2 receptor binding domain (RBD). It exhibits neutralizing activity against SARS-CoV-2 by binding to the RBD and the S-glycoprotein ectodomain and blocking S-glycoprotein-mediated binding to the receptor[1].
Pradimicin A (PRM-A) is a potent antifungal agent, with an MIC of 4 μg/mL against Candida rugosa. Pradimicin A has antiviral activities against CoV, HIV and other enveloped viruses. Pradimicin A shows aggregation property, and can recognize d-Man in the presence of Ca2+ ion[1][2].
SARS-CoV-2 Mpro-IN-9 (compound c7) is a nonpeptidic, noncovalent SARS-CoV-2 Mpro inhibitor (IC50=0.085 μM), with improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. SARS-CoV-2 Mpro-IN-9 inhibits viral replication (EC50=1.10 μM) in SARS-CoV-2-infected Vero E6 cells, while exhibits low cytotoxic effects (CC50>50 μM)[1].
Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is a autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
Ibuzatrelvir (PF-07817883) is an antiviral agent, targeting to SARS-CoV-2 3CL protease. Ibuzatrelvir can be used to inhibit COVID-19[1].
Bonducellpin D is a furanoditerpenoid lactone isolated from Caesalpinia minax. Bonducellpin D exhibits broad-spectrum inhibition potential against SARS-CoV Mpro and MERS-CoV Mpro, with an Ki of 467.11 and 284.86 nM, respectively. Bonducellpin D also exhibits moderate anti-cancer activity in vitro[1][2][3].
Antcin-B is a potent inhibitor of 3CLPro with high affinity. Antcin-B can be used in study SARS-CoV-2[1].
Remdesivir O-desphosphate acetonide impurity is an impurity of Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity and is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
SARS-CoV-2-IN-41 (compound 2) is a potent SARS-CoV-2 3CLpro inhibitor with an IC50 value of 0.022 µM. SARS-CoV-2-IN-41 shows antiviral effect[1].
(R)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine[1]. Hydroxychloroquine is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro[2][3][4].
Setrobuvir (ANA598) is an orally active non-nucleosidic HCV NS5B polymerase inhibitor. ANA-598 inhibits both de novo RNA synthesis and primer extension, with IC50s between 4 and 5 nM. Setrobuvir also shows excellent binding affinity to SARS-CoV-2 RdRp and induces RdRp inhibition[1][2].
(S)-Hydroxychloroquine ((S)-HCQ) is the enantiomer of Hydroxychloroquine[1]. Hydroxychloroquine, a synthetic antimalarial drug, inhibits Toll-like receptor 7/9 (TLR7/9) signaling, and shows efficiently inhibits SARS-CoV-2 infection in vitro[2][3][4].
SARS-CoV-2 nsp14-IN-3 (4975) is an inhibitor of the SARS-CoV-2 Nsp14 N7-Methyltransferase (IC50: 3.5 μM)[1].